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  • Title: Structure-activity relationship studies of CNS agents. XII. 1-[4-(4-aryl-1-piperazinyl)butyl]-3,4-dihydro-2(1H)-quinolinones: new 5-HT1A, 5-HT2 and D2 ligands with a potential antipsychotic activity.
    Author: Mokrosz JL, Chojnacka-Wójcik E, Dereń-Wesołek A, Kłodzińska A, Maćkowiak M, Bielecka Z, Paluchowska MH.
    Journal: Drug Des Discov; 1994 Apr; 11(3):197-203. PubMed ID: 7548635.
    Abstract:
    The synthesis of three 1-[4-(4-aryl-1-piperazinyl)butyl]-3,4-dihydro-2(1H)-quinolinones (5-7) was described and the receptor binding profile (5-HT1A, 5-HT2, alpha 1, D1, D2) was determined. It was found that m-chloro (5) and o-methoxy (6) derivatives are potent antagonists of the 5-HT1A, 5-HT2 and D2 receptors. It was shown that compound 6 resembles very well some atypical antipsychotics and may be considered as a novel agent of this class of drugs.
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